Drug intelligence / Profile preview

lapatinib + cisplatin

Development stage
Preclinical
Lead developer
GSK
Modality
Small Molecules
Administration
Oral (lapatinib), Intravenous (cisplatin)
01

Overview

**Lapatinib + cisplatin** is a combination of two antineoplastic agents used experimentally for the treatment of certain cancers, notably esophageal squamous cell carcinoma (ESCC) and in investigational regimens for muscle-invasive bladder cancer. Lapatinib is a small molecule tyrosine kinase inhibitor that targets the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), blocking their phosphorylation and downstream signaling via AKT and ERK, thus halting tumor growth and inducing apoptosis. Cisplatin is a platinum-based chemotherapeutic that causes DNA crosslinking, leading to cell cycle arrest and apoptosis. The combination acts synergistically to enhance cancer cell death, cell cycle arrest at G2/M phase, and apoptosis in vitro, particularly in cancers with EGFR/HER2 overexpression[1].

Brand names
Tykerb (for lapatinib)Platinol (for cisplatin)
02

Targets

ERBB2 (Erb-b2 receptor tyrosine kinase 2)ABCG2 (Breast cancer resistance protein)DNAEGFR T790M (Epidermal growth factor receptor T790M mutant)DDB2 (Damage-specific DNA-binding protein 2)

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